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In terms of the ring
2024-07-02

In terms of the ring B C5′ position, while C5′-F (compound ) was tolerated, C5′-Me (compound ) and C5′-Cl (compound ) substitutions resulted in a loss in potency. However, the C5′-OMe substitution (compound ) resulted in a ∼3-fold increase in potency compared to . Modeling suggested a pseudo hydroge
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The introduction of a pyrazole
2024-07-02

The introduction of a pyrazole moiety into any position of the sterane core by cross-coupling reactions [13] or by Knorr construction from a CCC bis-electrophilic sterane precursor and an N,N binucleophile building block [17], [19] may serve as an example. Very few reports are to be found, however,
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NGB 2904 A variety of quinazoline or
2024-07-02

A variety of quinazoline or fused pyrimidine-substituted diaminotriazoles showed sub-100nM inhibition of Axl (). Diaminotriazoles similarly substituted with quinolines, isoquinolines and benzothiazoles also showed potent Axl activity (data not shown), but generally exhibited potent cytotoxicity and
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The Kelch like ECH associated
2024-07-02

The Kelch-like ECH-associated protein 1 (Keap1)-Nrf2 signaling pathway functions as one of the key regulator of the cellular defense system against oxidative stress [26]. Nrf2 is a redox-sensitive transcription factor, that is sequestered in the cytoplam by binding to Keap1; however, under oxidative
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br Results br Discussion br Conclusions
2024-07-02

Results Discussion Conclusions In summary, this study provides novel report of pericardial adipose aromatase expression – in both human and rodent. We show that aromatase expression is remarkably upregulated with aging (Fig. 1C), and that total aromatase ha141 australia conversion capacity
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In our approach using BRET and
2024-07-02

In our approach using BRET and FRET, there is a substantial increase in BRET and FRET signals between Giα2 or Giα3-YFP and CFP- Gγ2/Rluc-Gγ2 upon apelin-13 activation, indicating that Gαi2, Gαi3 and N-terminus of Gβ1γ2 subunits become closer without subunit dissociation. In contrast, both the FRET a
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Plant defensins Vriens et al and linear AMPs
2024-07-02

Plant defensins (Vriens et al., 2014) and linear AMPs (Domingues et al., 2015, Liu et al., 2008) have been shown to present several modes of action. Among these different mechanisms, permeabilization of the fungal membrane has been described as a secondary effect of plant defensin action (Vriens et
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br Methods for antifungal testing of mucorales species
2024-07-02

Methods for antifungal testing of mucorales species The Clinical and Laboratory Standards Institute (CLSI) and European Committee on Antimicrobial Susceptibility Testing (EUCAST) reference methods currently in place for in vitro antifungal susceptibility testing of filamentous fungi [8], [9] have
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beta-Nicotinamide mononucleotide It has been well establishe
2024-07-02

It has been well established that shortly after systemic inflammation, NADPH oxidase and iNOS activity were increased in the beta-Nicotinamide mononucleotide and lead to overproduction of reactive oxygen species (ROS) and NO [66]. Moreover, previous studies indicated that Ang II induced an increase
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br Material and methods br Results br Discussion Nimodipine
2024-07-02

Material and methods Results Discussion Nimodipine administration inhibited the level of AMP-activated protein kinase (AMPK) phosphorylation, a sensor of cellular energy status that directs metabolic Calcium Gluceptate receptor to support cellular growth and survival. CCH influences the ox
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In a working group exposed month old transgenic mice mutatio
2024-07-01

In 2008, a working group exposed 12-month-old transgenic mice (mutation for human amyloid precursor protein expression) and their non-transgenic littermates to isoflurane and halothane for 120min per day for five days. It was concluded that in the transgenic mouse there was overload of amyloid prote
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An important and well documented
2024-07-01

An important and well-documented pathway involved in cellular growth and proliferation is the mTOR-mediated synthesis of proteins and lipids [7,13,14]. Although found to be tissue specific or context specific regulation, it has always been observed that either one or both the mTOR complexes regulate
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Corticosterone induced inhibition of OCT mediated
2024-07-01

Corticosterone-induced inhibition of OCT-mediated transport is rapid and appears to involve direct interaction of the steroid with the transporter at a specific site. Volk et al. (2003) studied OCT2-mediated transport by measuring substrate-induced currents using patch clamp of Xenopus oocytes exoge
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Perhaps the discovery of this linkage has served
2024-07-01

Perhaps the discovery of this linkage has served to catapult much of the work on ABCA1, leaving its family member in need of a relationship with a defined human pathology. In this regard, there is by now a quite mature literature that suggests that ABCA2 may have been overlooked in terms of its impo
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One study has demonstrated that PUFA
2024-07-01

One study has demonstrated that ω-3 PUFA reduced both cholesterol and caveolin-1 (a marker of raft), thereby displacing raft-associated signaling molecules from lipid raft [36]. Additionally, DHA treatment decreased the amount of lipid raft in the cell surface and displaced several lipid raft-associ
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